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Bioorg Med Chem Lett. 2004 Mar 22;14(6):1375-9.

Terephthalamide derivatives as mimetics of the helical region of Bak peptide target Bcl-xL protein.

Author information

1
Department of Chemistry, Yale University, PO Box 20810, New Haven, CT 06511, USA.

Abstract

A group of novel Bcl-xL/Bak antagonists, based on a terephthalamide scaffold, were designed to mimic the alpha-helical region of the Bak peptide. Good in vitro inhibition potencies in disrupting the Bak/Bcl-xL complex have been observed (terephthalamide 4, K(i)=0.78+/-0.07 microM).

PMID:
15006365
DOI:
10.1016/j.bmcl.2003.09.096
[Indexed for MEDLINE]

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